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The synthesis of endothelin (ET) in vascular endothelial cells is complex, beginning with preproendothelin, a large precursor molecule. Preproendothelin is processed by furin-like proteases into biologically inactive big endothelins,1 and finally converted by ET-converting enzyme (ECE) to fully active ET.2 |
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Once released from the endothelium, ET exerts its effects through binding to two receptors, ETA and ETB. The consequences of binding differ according to the cell type on which the receptors are found. |
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REFERENCES |
1. |
Kedzierski RM, Yanagisawa M. Endothelin system: the double-edged sword in health and disease. Ann Rev Pharmacol Toxicol. 2001;41:851–876. |
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2. |
Braunwald E, Zipes DP, Libby P, eds. Heart Disease. 2 vols. 6th ed. Philadelphia, PA: WB Saunders Co; 2001:1096.
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3. |
Panza JA, Cannon RO, eds. Endothelium, Nitric Oxide, and Atherosclerosis: From Basic Mechanisms to Clinical Implications. Armonk, NY: Futura; 1999. |
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4. |
Rae GA, Henriques MGMO. Endothelins in inflammation. In Said SI, ed. Proinflammatory and Antiinflammatory Peptides. New York: Marcel Dekker Inc; 1998:163–202. Lenfant C, ed. Lung Biology in Health and Disease, vol. 112. |
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5. |
Davie N, Haleen SJ, Upton PD, et al. ET(A) and ET(B) receptors modulate the proliferation of human pulmonary artery smooth muscle cells. Am J Respir Crit Care Med. 2002;165:398–405. |
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6. |
Piacentini L, Gray M, Honbo NY, et al. Endothelin-1 stimulates cardiac fibroblast proliferation through activation of protein kinase C. J Mol Cell Cardiol. 2000;32:565–576. |
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7. |
Katwa LC, Guarda E, Weber KT. Endothelin receptors in cultured adult rat cardiac fibroblasts. Cardiovasc Res. 1993;27:2125–2129. |
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© 2008 Actelion Pharmaceuticals US, Inc. All rights reserved. |
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